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1. 发明申请

WO2006136859A2 INDOLIZINE DERIVATIVES 审中-公开
标题翻译：吲哚衍生物
公开(公告)号：WO2006136859A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002341
申请日：2006-06-26
申请人： ARGENTA DISCOVERY LTD. , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R 1 , R 2 , R 3 and R 4 each independently are hydrogen, C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl, halo, -S(O) n R 10 , -SO 2 N(R 10 ) 2 , -N(R 10 ) 2 , -C(O)N(R 10 ) 2 , -NR 10 C(O)R 9 , -CO 2 R 10 , -C(O)R 9 , -NO 2 , -CN or -OR 11 ; wherein each R 9 is independently C 1 C 6 alkyl, aryl, heteroaryl; R 10 is independently hydrogen, C 1 C 6 alkyl, aryl, or heteroaryl; R 11 is hydrogen, C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl or a group -SO 2 R 9 ; n is 0, 1 or 2; R5 is C 1 C 6 alkyl, fully or partially fluorinated C 1 C 6 alkyl , C 1 C 6 alkenyl , C 1 C 6 alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R 6 is hydrogen, C 1 C 6 alkyl or fully or partially fluorinated C 1 C 6 alkyl ; R 7 and R 8 are independently hydrogen or C 1 C 6 alkyl, or R 7 and R 8 together with the atom to which they are attached form a cycloalkyl group; and X is -CHR 6 -, -S(O) n -, -NR 6 SO 2 - or -SO 2 NR 6 - wherein n is 0, 1 or 2.
摘要翻译：式（I）化合物是CRTH2受体的配体，可用于治疗呼吸系统疾病：式（I）其中R 1，R 2，R SUB > 3和R 4各自独立地是氢，C 1 -C 6烷基，完全或部分氟化的C 1 C 6烷基，卤素，-S（O）n R 10，-SO 2 N， N（R 10）2，-N（R 10）2 - ， - C（O）N（R 10） R 10，-NR 10 C（O）R 9，-CO 2， R 10，-C（O）R 9，-NO 2，-CN或-OR 11， SUB>; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化C 1 -C 6 烷基或基团-SO 2 R 9; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化的C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 1个C 6链烯基，C 1 -C 6炔基，任选取代的芳基或任选取代的杂芳基; R 6是氢，C 1 -C 6烷基或完全或部分氟化的C 1 -C 6 烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或R 7， / SUB和R 8与它们所连接的原子一起形成环烷基; 并且X是-CHR 6 - ， - S（O）n - ， - NR 6 SO 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

2. 发明申请

WO2008074966A1 CRTH2 ANTAGONISTS 审中-公开
公开(公告)号：WO2008074966A1
公开(公告)日：2008-06-26
申请号：PCT/GB2006/004856
申请日：2006-12-21
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MIDDLEMISS, David , CRAMP, Michael, Colin , BLANEY, Paul, Matthew , WILLIAMS, Karen , GRIFFON, Yan , HARRISON, Trevor, Keith , CRACKETT, Peter
IPC分类号： A61K31/437 , C07D471/04 , A61P37/08
CPC分类号： C07D471/04
摘要： The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, ( R )-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, ( S )-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(6-fluoroquinolin-2-ylmethyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-bromophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, and [3-(4-cyclopropylsulfamoylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid.
摘要翻译：以下化合物是可用于治疗呼吸系统疾病的CRTH2拮抗剂：[3-（2,4-二氯苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（2- （4-甲基磺酰基-2-三氟甲基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸，（R） - （4-氟-4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基] 2- [6-氟-3-（4-甲磺酰基苯基硫基）-2-甲基吲哚啉-1-基]丙酸，[3-（4-乙磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸，（S）-2- [6-氟-3-（4-甲磺酰基苯基硫烷基）-2-甲基吲哚啉-1-基]丙酸，乙磺酰氨基苯磺酰基）-6-氟-2-甲基吲哚啉-1-基]乙酸[7 （4-甲磺酰基苯基硫烷基）-2-甲基吲哚哩啶-1-基]乙酸[3-（2-氯-4-甲磺酰基苯基硫烷基）-7-氰基-2-甲基吲哚啉-1-基] ]乙酸，[6-氰基-3-（4-甲磺酰基苄基）-2-甲基吲哚啉-1-基]乙酸[3-（4-氯苄基）-7-氰基-2-甲基吲哚吡啶-1-基]乙酸[6-氰基-3-（6-氟喹啉-2-基甲基）-2-甲基吲哚啉-1-基]乙酸[6-氟-3-（4-甲氧基苯基硫烷基） 2-甲基吲哚啉-1-基]乙酸，[7-氯-6-氟-3-（4-甲氧基苯基硫烷基）-2-甲基吲哚啉-1-基]乙酸，[3-（4-溴苯基硫烷基）-6- -2-氟-2-甲基吲哚啉-1-基]乙酸和[3-（4-环丙基氨磺酰基苯基硫烷基）-6-氟-2-甲基吲哚啉-1-基]乙酸。

3. 发明申请

WO2007036743A3 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：WO2007036743A3
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003644
申请日：2006-09-29
申请人： ARGENTA DISCOVERY LTD. , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
发明人： CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary
IPC分类号： A61K31/47 , A61P11/00 , A61P43/00 , C07D215/00
摘要： Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component; in which: R 1 , R 2 , R 3 , R 4 and R 5 are independently hydrogen, C 1 -C 6 alkyl, C 1 - C 6 fluoroalkyl, cyclopropyl, halo, -S(O) n R 6 , -SO 2 NR 7 R 8 , -NR 7 R 8 , -NR 7 C(O)R 6 , -CO 2 R 7 , -C(O)NR 7 R 8 , -C(O)R 6 , -NO 2 , -CN or a group -OR 9 ; wherein each R 6 is independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, aryl, or heteroaryl; R 7 , R 8 are independently C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cycloalkyl-(C 1 -C 6 alkyl)-, aryl, heteroaryl or hydrogen; R 9 is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 fluoroalkyl, cycloalkyl, cylcoalkyl-(C 1 -C 6 alkyl)-, or a group -SO 2 R 6 ; A is -CHR 10 -, -C(O)-, -S(O) n -, -0-, or -NR 10 - wherein n is an integer from 0-2 and R 10 is hydrogen, C 1 -C 3 alkyl, or C 1 -C 6 fluoroalkyl group; B is a direct bond, or a divalent radical selected from -CH 2 -, -CH 2 CH 2 -, -CHR 11 -, -CR 11 R 12 -, -CH 2 CHR 11 -, -CH 2 CR 11 R 12 -, -CHR 11 CHR 12 -, and divalent radicals of formula -(CR 11 R 12 ) P -Z- wherein Z is attached to the ring carrying R 1 , R 2 and R 3 ; wherein R 11 is C 1 -C 3 alkyl, cyclopropyl, C 1 -C 6 fluoroalkyl; R 12 is methyl or fluoromethyl; p is independently 1 or 2; and Z is -0-, -NH-, or -S(O) n -, wherein n is an integer from 0-2; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, or sulfonic acid group, or a group of formula C(=O)NHSO 2 R 6 or SO 2 NHC(=O)R 6 ; and Y is aryl, heteroaryl, aryl-fused- heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group.

4. 发明申请

WO2007031747A1 IMDOLIZINE DERIVATIVES AS LIGANDS OF THE CRTH2 RECEPTOR 审中-公开
标题翻译：作为CRTH2受体配体的咪唑啉衍生物
公开(公告)号：WO2007031747A1
公开(公告)日：2007-03-22
申请号：PCT/GB2006/003394
申请日：2006-09-14
申请人： ARGENTA DISCOVERY LTD. , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are CRTH2 antagonists, useful in the treatment of, for example, asthma, chronic obstructive pulmonary disease, rhinitis, allergic airway syndrome, and allergic rhinobronchitis. Formula (I) wherein R 1 , R 2 . R 3 and R 4 each independently are hydrogen, C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl, halo, -S(O) n R 10, -SO 2 N(R 10 ) 2, -N(R 10 ) 2, -C(O)N(R 10 ) 2, -NR 10 C(O)R 9, -CO 2 R 10 , -C(O)R 9 , -NO 2, -CN or -OR 11 ; wherein each R 9 is independently C 1 -C 6 alkyl, aryl, heteroaryl; R 10 is independently hydrogen, C 1 -C 6 alkyl, aryl, or heteroaryl; R 11 is hydrogen, C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl or a group -SO 2 R 10 ; n is 0, 1 or 2; R 5 is C 1 -C 6 alkyl, fully or partially fluorinated C 1 -C 6 alkyl, C 1 -C 6 alkenyl, C 1 -C 6 alkynyl, optionally substituted aryl, or optionally substituted heteroaryl; R 6 is hydrogen, C 1 -C 6 alkyl or fully or partially fluorinated C 1 -C 6 alkyl ; R 7 and R 8 are independently hydrogen or C 1 -C 6 alkyl, or R 7 and R 8 together with the atom to which they are attached form a cycloalkyl group; and X is -CHR 6 -, -S(O) n -, -C(O)-, -NR 6 SO 2 - or -SO 2 NR 6 - wherein n is 0, 1 or 2.
摘要翻译：式（I）化合物是CRTH2拮抗剂，可用于治疗例如哮喘，慢性阻塞性肺病，鼻炎，过敏性气道综合征和过敏性鼻炎支原体炎。式（I）其中R 1，R 2， R 3和R 4各自独立地是氢，C 1 -C 6烷基，完全或部分氟化的C C 1 -C 6烷基，卤素，-S（O）n R 10，-SO 2 - ， - 2 N（R 10）2，-N（R 10）2， - C （O）N（R 10）2，-NR 10 C（O）R 9，-CO -C（O）R 9，-NO 2，-CN或-OR 2， SUB> 11 ; 其中每个R 9独立地是C 1 -C 6烷基，芳基，杂芳基; R 10独立地是氢，C 1 -C 6 -C 6烷基，芳基或杂芳基; R 11是氢，C 1 -C 6烷基，完全或部分氟化的C 1 -C 3 > 6个或多个烷基或基团-SO 2 R 10; n为0,1或2; R 5是C 1 -C 6烷基，完全或部分氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6烷基，C 1 -C 6亚烯基，C 1 -C 6 - 炔基，任选取代的芳基或任选取代的杂芳基; R 6是氢，C 1 -C 6烷基或完全或部分氟化的C 1 -C 3 > 6个烷基; R 7和R 8独立地是氢或C 1 -C 6烷基，或R 7 R 3和R 8与它们所连接的原子一起形成环烷基; 并且X是-CHR 6 - ， - S（O）n - ， - C（O） - ， - NR 6 SO > 2 - 或-SO 2 NR 6 - ，其中n为0,1或2。

5. 发明申请

WO2008119917A1 QUINOLINE DERIVATIVES AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译：喹啉衍生物作为CRTH2受体配体
公开(公告)号：WO2008119917A1
公开(公告)日：2008-10-09
申请号：PCT/GB2007/001138
申请日：2007-03-29
申请人： ARGENTA DISCOVERY LIMITED , RAY, Nicholas, Charles , FINCH, Harry , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , MONTANA, John, Gary
发明人： RAY, Nicholas, Charles , FINCH, Harry , CRAMP, Michael, Colin , ARIENZO, Rosa , HYND, George , CRACKETT, Peter , GRIFFON, Yann , HARRISON, Trevor, Keith , MONTANA, John, Gary
IPC分类号： C07D215/20 , C07D215/22 , A61K31/47 , A61P11/00 , A61P29/00
CPC分类号： C07D215/233 , C07D215/20 , C07D215/227
摘要： Specific quinoline derivatives are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory component.
摘要翻译：特定的喹啉衍生物是可用于治疗具有炎性成分的病症的CRTH2拮抗剂。

6. 发明申请

WO2008113965A1 INDOLIZINE ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS 审中-公开
标题翻译：将醋酸衍生物作为CRTH2拮抗剂
公开(公告)号：WO2008113965A1
公开(公告)日：2008-09-25
申请号：PCT/GB2007/000996
申请日：2007-03-21
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
发明人： HYND, George , RAY, Nicholas, Charles , FINCH, Harry , MONTANA, John, Gary , CRAMP, Michael, Colin , HARRISON, Trevor, Keith , ARIENZO, Rosa , BLANEY, Paul , GRIFFON, Yann , MIDDLEMISS, David
IPC分类号： A61K31/437 , C07D471/04 , A61P11/00
CPC分类号： C07D471/04
摘要： The specific compounds of this list : {7-cyano-2-methyl-1-[4-(morpholine-4-sutfonyl)benzyl]indolizin-3-yl}acetic acid, {1 -(3-chloro-4-ethanesulfonylbenzyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro4-(morpholine-4-sulfonyl)benzyl]-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-(3-chloro-4-ethanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-3-yl}acetic acid, {1-[3-chloro-4-(morpholine-4-sutfonyl)phenylsutfanyl]-7-cyano-2-methylindolizin-3- yl}acetic acid, {7-cyano-1 -(6-fluoroquinolin-2-y1methyl)-2-methylindolizin-3-yl}acetic acid are ligands of the CRTH2 receptor and are useful in the treatment of respiratory diseases.
摘要翻译：该列表的具体化合物：{7-氰基-2-甲基-1- [4-（吗啉-4-磺酰基）苄基]中氮茚-3-基}乙酸，{1-（3-氯-4-乙磺酰基苄基）-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-（吗啉-4-磺酰基）苄基] -7-氰基-2-甲基吲哚啉-3-基}乙酸， {1-（3-氯-4-乙磺酰基苯基硫烷基）-7-氰基-2-甲基吲哚啉-3-基}乙酸{1- [3-氯-4-（吗啉-4-磺基）苯基f烷基] 氰基-2-甲基吲哚啉-3-基}乙酸，{7-氰基-1-（6-氟喹啉-2-基甲基）-2-甲基吲哚啉-3-基}乙酸是CRTH2受体的配体，可用于治疗呼吸系统疾病。

7. 发明申请

WO2007045867A1 3 -AMINOINDOLE COMPOUNDS AS CRTH2 RECEPTOR LIGANDS 审中-公开
标题翻译： 3 -AMINOINDOLE化合物作为CRTH2受体配体
公开(公告)号：WO2007045867A1
公开(公告)日：2007-04-26
申请号：PCT/GB2006/003872
申请日：2006-10-18
申请人： ARGENTA DISCOVERY LTD. , RAY, Nicholas, Charles , HYND, George , ARIENZO, Rosa , FINCH, Harry
发明人： RAY, Nicholas, Charles , HYND, George , ARIENZO, Rosa , FINCH, Harry
IPC分类号： C07D209/40 , A61K31/405 , A61P29/00
CPC分类号： C07D209/40
摘要： Compounds of formula [I] are CRTH2 antagonists, useful in the treatment o conditions having an inflammatory component: in which: R 1 , R 2 , R 3 and R 4 are independently hydrogen, (C 1 -C 6 ) alky!, (C 1 -C 6 ) haloalkyl, halo, -S(O) n R 10 , -NR 11 SO 2 R 10 , -SO 2 N(R 11 ) 2 , -N(R 11 ) 2 , -NR 11 C(O)R 10 , -C(O)N(R 11 ) 2 , -CO 2 R 11 , -C(O)R 10 , CN or a group OR 12 ; wherein each R 10 is independently (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, aryl, or heteroaryl; R 11 is independently hydrogen, (C 1 -C 6 )alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, aryl, or heteroaryl; R 12 is hydrogen, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, cycloalkyl, or a group -SO 2 R 10 , wherein n is O 1 or 2; R 5 and R 6 are independently hydrogen, (C 1 -C 6 ) alkyl or (C 1 -C 6 ) haloalkyl, or R 5 and R 6 together with the atom to which they are attached form a cycloalkyl group; R 7 is hydrogen, (C 1 -C 6 ) alkyl, or (C 1 -C 6 ) haloalkyl; R 8 is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused- heterocycloalkyl or aryl-fused-cycloalkyl; and R 9 is hydrogen, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, or cycloalkyl.
摘要翻译：式[I]化合物是CRTH2拮抗剂，可用于治疗具有炎性成分的条件：其中：R 1，R 2，R 3， R 4和R 4独立地是氢，（C 1 -C 6）烷基（C 1 -C 6）烷基，卤代烷基，卤素，-S（O）n R 10，-NR 11，SO 2， 2，N 2，N 2，N 2，R 2，R 2， N（R 11）2，-NR 11 C（O）R 10，-C（O） N（R 11）2，-CO 2 R 11，-C（O）R 11， 10，CN或基团OR 12; 其中每个R 10独立地为（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - C 卤代烷基，环烷基，芳基或杂芳基; R 11独立地是氢，（C 1 -C 6 -C 6）烷基，（C 1 -C 6亚烷基）卤代烷基，环烷基，芳基或杂芳基; R 12是氢，（C 1 -C 6 - ）烷基，（C 1 -C 6 - 6个）卤代烷基，环烷基或基团-SO 2 R 10，其中n是O 1或2; R 5和R 6独立地是氢，（C 1 -C 6 -C 6）烷基或（C _{1个C 6 -C 6卤代烷基或R 5和R 6和它们所连接的原子一起形成一个环烷基 R 7是氢，（C 1 -C 6 -C 6）烷基，或（C 1 -C 3 - C > 6个）卤代烷基; R 8是芳基，杂芳基，芳基稠合 - 杂环烷基，杂芳基 - 稠合环烷基，杂芳基 - 稠合 - 杂环烷基或芳基稠合环烷基; 并且R 9是氢，（C 1 -C 6 -C 6）烷基，（C 1 -C 6 - C > 6个）卤代烷基或环烷基。}

8. 发明申请

WO2008122784A1 QUINOLINES AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：喹啉及其治疗用途
公开(公告)号：WO2008122784A1
公开(公告)日：2008-10-16
申请号：PCT/GB2008/001201
申请日：2008-04-03
申请人： ARGENTA DISCOVERY LIMITED , MONTANA, John, Gary , FINCH, Harry , HYND, George , CRAMP, Michael, Colin , ARIENZO, Rosa , MCLEAN, Neville
发明人： MONTANA, John, Gary , FINCH, Harry , HYND, George , CRAMP, Michael, Colin , ARIENZO, Rosa , MCLEAN, Neville
IPC分类号： C07D401/10 , C07D413/10 , C07D417/10 , C07D215/227 , C07D215/233 , A61K31/4709 , A61P11/00
CPC分类号： C07D401/10 , C07D215/227 , C07D215/233 , C07D413/10 , C07D417/10
摘要： Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: R 1 is halogen or cyano; R 2 is hydrogen or methyl; R 3 and R 4 are independently -OR 6 , C 1 -C 6 alkyl or C 3 -C 6 cycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; R 5 is hydrogen or halogen; R 6 is C 1 C 6 alkyl or C 3 -C 6 cycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is -CH 2 -, -S-, or -O-; one of Y and Y 1 is hydrogen and the other is OR 6 , -C(=O)R 7 , NR 8 SO 2 R 6 or a heterocyclic group selected from those referred to in the specification; and R 6 , R 7 and R 8 are as defined in the specification.
摘要翻译：式（I）化合物是可用于治疗例如哮喘和COPD的CRTH2配体，其中：R 1是卤素或氰基; R 2是氢或甲基; R 3和R 4独立地为-OR 6，C 1 -C 6 >烷基或C 3 -C 6环烷基，后两个基团任选地被一个或多个卤素原子取代; R 5是氢或卤素; R 6是C 1 -C 6烷基或C 3 -C 6 - 环烷基其中任一个任选被一个或多个卤素原子取代; X是-CH 2 - ， - S-或-O-; Y和Y 1之一是氢，另一个是OR 6，-C（= O）R 7，NR 8 或者选自本说明书中提及的那些的杂环基;和/或和R 6，R 7和R 8是如说明书中所定义的。

9. 发明申请

WO2010040989A1 QUINOLIN-2-ONE COMPOUNDS 审中-公开
标题翻译：喹啉-2-酮化合物
公开(公告)号：WO2010040989A1
公开(公告)日：2010-04-15
申请号：PCT/GB2009/002368
申请日：2009-10-05
申请人： ARGENTA ORAL THERAPEUTICS LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , WARD, Stuart
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , WARD, Stuart
IPC分类号： C07D401/06 , C07D417/06 , C07D215/227
CPC分类号： C07D215/227 , C07D401/06 , C07D417/06
摘要： A compound of structural formula [1]: in which: A represents a direct bond, an optionally substituted alkylene or alkenylene group, or a group of formula Z-(optionally substituted)alkylene; B represents a direct bond, an optionally substituted alkylene or alkenylene group, or a group of formula Z-(optionally substituted)alkylene or (optionally substituted)alkylene-Z; Z represents an oxygen atom, an NH or N-alkyl group, a group of formula S(O) n , in which n = 0 to 2, or a group of formula -O-SO 2 -; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(=O)NHSO 2 W or SO 2 NHC(=O)W; W represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl group; Y represents an optionally substituted aryl or heteroaryl group, or an optionally substituted aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl, aryl-fused-cycloalkyl or cycloalkyl group; R a , R b and R c independently represent hydrogen, acyl, alkoxy, alkylsulphinyl, alkylsulphonyl, alkylthio, -NH 2 , aminoalkyl, hydroxyalkyl, arylalkyl, cyano, dialkylamino, halo, haloalkoxy, haloalkyl, alkyl, alkenyl, -OH, -CHO, -NO 2 , aryl (optionally substituted with alkoxy, haloalkoxy, halogen, alkyl or haloalkyl), heteroaryl (optionally substituted with alkoxy, haloalkoxy, halogen, alkyl or haloalkyl), heterocycloalkyl, aminoacyl, aminosulphonyl, acylamino, sulphonylamino, heteroarylalkyl, cyclic amine, aryloxy, heteroaryloxy, arylalkyloxy or heteroarylalkyloxy;
摘要翻译：结构式[1]的化合物：其中：A表示直接键，任选取代的亚烷基或亚烯基，或式Z-（任选取代的）亚烷基; B表示直接键，任选取代的亚烷基或亚烯基，或式Z-（任选取代的）亚烷基或（任选取代的）亚烷基-Z的基团; Z表示氧原子，NH或N-烷基，其中n = 0至2的式S（O）n基团，或式-O-SO 2基团; X表示羧酸，四唑，3-羟基异恶唑，异羟肟酸，次膦酸盐，膦酸盐，膦酰胺，磺酸或式C（= O）NHSO 2 W或SO 2 NHC（= O）W的基团; W表示任选取代的芳基或杂芳基或任选取代的烷基; Y表示任选取代的芳基或杂芳基，或任选取代的芳基稠合 - 杂环烷基，杂芳基 - 稠合 - 环烷基，杂芳基 - 稠合 - 杂环烷基，芳基 - 稠合环烷基或环烷基; R a，R b和R c独立地表示氢，酰基，烷氧基，烷基亚磺酰基，烷基磺酰基，烷硫基，-NH 2，氨基烷基，羟基烷基，芳基烷基，氰基，二烷基氨基，卤素，卤代烷氧基，卤代烷基，烷基，烯基，-OH，-CHO，，芳基（任选被烷氧基，卤代烷氧基，卤素，烷基或卤代烷基取代），杂芳基（任选被烷氧基，卤代烷氧基，卤素，烷基或卤代烷基取代），杂环烷基，氨基酰基，氨基磺酰基，酰氨基，磺酰氨基，杂芳基烷基，环胺，芳氧基，杂芳氧基，芳基烷氧基或杂芳基烷氧基;

10. 发明申请

WO2009044147A1 INDOLIZINE DERIVATIVES WITH CRTH2 RECEPTOR AFFINITY FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：具有CRTH2受体亲和力的吲哚美辛衍生物用于治疗炎症性疾病
公开(公告)号：WO2009044147A1
公开(公告)日：2009-04-09
申请号：PCT/GB2008/003345
申请日：2008-10-02
申请人： ARGENTA DISCOVERY LIMITED , HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , GOLD, Johan , CARNEVALE, Gennaro
发明人： HYND, George , MONTANA, John, Gary , FINCH, Harry , CRAMP, Michael, Colin , GOLD, Johan , CARNEVALE, Gennaro
IPC分类号： C07D471/04 , A61K31/437 , A61P11/00
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are ligands of the CRTH2 receptor, useful in the treatment of, for example, inflammatory respiratory disease: R 1 is fluoro, chloro, CN or CF 3 ; R 2 is hydrogen, fluoro or chloro; X is -CH 2 -, or - S(O) n -; Ar 1 is phenyl or 5- or 6-membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted with one substituent selected from fluoro, chloro, CN, -O(C 1 -C 3 alkyi) or C 1 -C 3 alkyl, the latter two groups being optionally substituted by one or more fluoro atoms; Y is -CR 3 R 4 -, -C(O)-, -O-, -S(O) 2 - or -NR 3 -; R 3 and R 4 independently represent hydrogen or C 1 -C 3 alkyl; Ar 2 is phenyl or 5- or 6- membered heteroaryl, wherein the phenyl or heteroaryl rings are optionally substituted by one or more substituents independently selected from halogen, - CN, -S(O) n R 5 , -S(O) 2 NR 6 R 7 , -NR 6 S(O) 2 R 5 -NR 6 R 7 , -NR 6 COR 5 , -CONR 6 R 7 , -COR 5 , -OR 6 , C 1 - C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; R 5 is C 1 -C 6 alkyl or C 3 -C 7 cycloalkyl, optionally substituted by one or more fluoro atoms; R 6 and R 7 independently represent hydrogen, C 1 -C 6 alkyl or C 3 -C 7 cycloalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and n is O, 1 or 2.
摘要翻译：式（I）化合物是CRTH2受体的配体，可用于治疗例如炎性呼吸系统疾病：R1是氟，氯，CN或CF3; R2是氢，氟或氯; X是-CH 2 - 或-S（O）n - ; Ar1为苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选被一个选自氟，氯，CN，-O（C 1 -C 3烷基）或C 1 -C 3烷基的取代基取代，后两个基团任选被一个或多个氟原子取代; Y是-CR 3 R 4 - ， - C（O） - ， - O - ， - S（O）2 - 或-NR 3 - ; R3和R4独立地表示氢或C1-C3烷基; Ar 2是苯基或5-或6-元杂芳基，其中苯基或杂芳基环任选地被一个或多个独立地选自卤素，-CN，-S（O）nR 5，-S（O）2 NR 6 R 7，-NR 6 S （O）2R5 -NR6R7，-NR6COR5，-CONR6R7，-COR5，-OR6，C1- C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; R5是任选被一个或多个氟原子取代的C 1 -C 6烷基或C 3 -C 7环烷基; R6和R7独立地表示氢，C1-C6烷基或C3-C7环烷基，后两个基团任选被一个或多个氟原子取代; 并且n为O，1或2。

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